| Identification | Back Directory | [Name]
LSD1-IN-7 Methylbenzenesulfonate | [CAS]
2097523-57-2 | [Synonyms]
LSD1-IN-7 Methylbenzenesulfote
LSD1-IN-7 Methylbenzenesulfonate
Pulrodemstat Methylbenzenesulfonate | [Molecular Formula]
C31H31F2N5O5S | [MDL Number]
MFCD32263407 | [MOL File]
2097523-57-2.mol | [Molecular Weight]
623.68 |
| Hazard Information | Back Directory | [Uses]
CC-90011 Methylbenzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 Methylbenzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 Methylbenzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity[1]. | [in vivo]
CC-90011 (5 mg/kg; oral administration; daily; for 30 days; for 30 days) treatment inhibits tumor growth in patient-derived xenograft SCLC models[1].
CC-90011 (once a day; for 4 days) treatment results in robust downregulation of GRP mRNA levels at 2.5 mg/kg and maximum suppression of GRP at 5 mg/kg in a SCLC human tumor xenograft (H1417) mice[1].
After i.v. administration, CC-90011 (Compound 11; 5 mg/kg) has systemic clearance of 32.4 mL/min/kg, elimination half-life of 2 h, and a high volume of distribution of 7.5 L/kg. CC-90011 (Compound 11; 5 mg/kg) is readily absorbed after oral administration with an AUC0-24h of 1.8 μM·h, C/sub>max of 0.36 μM, and oral bioavailability of 32%[1]. | Animal Model: | BALB/c nude mice bearing small cell lung carcinoma (SCLC)[1] | | Dosage: | 5 mg/kg | | Administration: | Oral administration; daily; for 30 days | | Result: | Showed a tumor growth inhibition (TGI) of 78% at 5 mg/kg with no body weight loss. |
| [IC 50]
KDM1/LSD1 | [References]
[1] Toufike Kanouni, et al. Discovery of CC-90011: A Potent and Selective Reversible Inhibitor of Lysine Specific Demethylase 1 (LSD1). J Med Chem. 2020 Dec 10;63(23):14522-14529. DOI:10.1021/acs.jmedchem.0c00978 |
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